61150-57-0Relevant articles and documents
Aromatic amine derivative organic electroluminescent material and device thereof
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Paragraph 0268-0271, (2021/11/26)
The invention discloses an aromatic amine derivative organic electroluminescent material and a device thereof. The compound is a pyrene compound substituted with an aromatic amine, wherein the compound has a substituted or unsubstituted (hetero) aryl group and a pyrene compound substituted or unsubstituted aromatic amine structure of a (hetero) aryl group, which may be used as a light emitting material in an organic electroluminescent device. These novel compounds can provide better device performance, such as higher external quantum efficiency and narrower half-peak widths, and the like.
QUINOXALINE DERIVATIVES
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Page/Page column 86, (2021/07/24)
The present invention relates to compounds according to general formula (I), which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
SPIROCYCLIC TETRAHYDROQUINAZOLINES
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Paragraph 0538-0539, (2021/07/17)
Provided are compounds represented by Formula I, wherein R3, A, A1, A2, A3, E, E1, E2, L, Q, Z, and (aa) are as defined in the specification, and the pharmaceutically acceptable salts and solvates thereof. Compounds of Formula (I) are KRAS inhibitors and are thus useful to treat cancer and other diseases.
Spirocyclic tetrahydroquinazolines
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Paragraph 0743; 0746-0748, (2021/07/11)
The invention discloses spirocyclic tetrahydroquinazolines , and particularly provide compounds represented by Formula I shown in the specification, and pharmaceutically acceptable salts and solvates thereof. In the formula, R3, A, A1, A2, A3, E, E1, E2, L, Q, Z and a structure shown in the specification are as defined in the specification,. The compounds of formula I are KRAS inhibitors and are therefore useful in the treatment of cancer and other diseases.
Cross-coupling strategy for the synthesis of diazocines
Eleya, Nadi,Li, Shuo,Staubitz, Anne
supporting information, p. 1624 - 1627 (2020/03/13)
Ethylene bridged azobenzenes are novel, promising molecular switches that are thermodynamically more stable in the (Z) than in the (E) configuration, contrary to the linear azobenzene. However, their previous synthetic routes were often not general, and yields were poorly reproducible, and sometimes very low. Here we present a new synthetic strategy that is both versatile and reliable. Starting from widely available 2-bromobenzyl bromides, the designated molecules can be obtained in three simple steps.
tBuOK-Promoted Cyclization of Imines with Aryl Halides
Li, Ya-Wei,Zheng, Hong-Xing,Yang, Bo,Shan, Xiang-Huan,Qu, Jian-Ping,Kang, Yan-Biao
supporting information, p. 4553 - 4556 (2020/06/08)
A transition-metal-free indole synthesis using radical coupling of 2-halotoluenes and imines via the later-stage C-N bond construction was reported for the first time. It includes an aminyl radical generation by C-H cleaving addition of 2-halotoluenes to imines via the carbanion radical relay and an intramolecular coupling of aryl halides with aminyl radicals. One standard condition can be used for all halides including F, Cl, Br, and I. No extra oxidant or transition metal is required.
Regiocontrolled and Stereoselective Syntheses of Tetrahydrophthalazine Derivatives using Radical Cyclizations
Zhang, Wei,Mo, Jia Yi,He, Weiying,Kennepohl, Pierre,Sammis, Glenn M.
supporting information, p. 976 - 980 (2019/01/04)
Tetrahydrophthalazine derivatives have found important applications in pharmaceutical research, but existing synthetic methods are unable to access them regio- and stereoselectively. Here, a new approach is presented that addresses these challenges by utilizing a 6-endo-trig radical cyclization in the key step. The desired tetrahydrophthalazines can be accessed in high yields (55–98 %) and high diastereoselectivities for the trans-product (>95:5) starting either from readily accessible hydrazones, or from the corresponding aldehydes and substituted Boc-hydrazides in a one-pot process. The synthetic versatility of the tetrahydrophthalazine core was demonstrated by its straightforward conversion to dihydro-phthalazines, phthalazines, or pyrazolo dione derivatives. Furthermore, the N?N bond was reduced to afford a new route to 1,4-diamines.
Strategy for Overcoming Full Reversibility of Intermolecular Radical Addition to Aldehydes: Tandem C-H and C-O Bonds Cleaving Cyclization of (Phenoxymethyl)arenes with Carbonyls to Benzofurans
Zheng, Hong-Xing,Shan, Xiang-Huan,Qu, Jian-Ping,Kang, Yan-Biao
supporting information, p. 3310 - 3313 (2018/06/11)
An intermolecular addition of carbon radicals enabled by a cascade radical coupling strategy is developed. It includes an intermolecular alkyl radical addition to a carbonyl group followed by an intramolecular alkoxy radical addition to haloarenes and produces substituted benzofurans in high yields. The radical nature of this reaction is explored by radical trapping experiments and EPR analysis. The mechanism is investigated by KIE experiments and control experiments. This method could provide rapid and practical access to the key intermediate of TAM-16, a safe and potent antibacterial agent for treating tuberculosis, and, therefore, is of great importance for organic synthesis and the pharmaceutical industry.
Rhodium-Catalyzed, Enantioselective Hydroacylation of ortho-Allylbenzaldehydes
Johnson, Kirsten F.,Schmidt, Adam C.,Stanley, Levi M.
supporting information, p. 4654 - 4657 (2015/10/12)
The development of a rhodium catalyst for endo- and enantioselective hydroacylation of ortho-allylbenzaldehydes is reported. A catalyst generated in situ from [Rh(COD)Cl]2, (R)-DTBM-SEGPHOS, and NaBARF promotes the desired hydroacylation reactions and minimizes the formation of byproducts from competitive alkene isomerization and ene/dehydration pathways. These rhodium-catalyzed processes generate the 3,4-dihydronaphthalen-1(2H)-one products in moderate-to-high yields (49-91%) with excellent enantioselectivities (96-99% ee).
Synthesis of N-alkoxyindol-2-ones by copper-catalyzed intramolecular N-arylation of hydroxamates
Kukosha, Tatyana,Trufilkina, Nadezhda,Katkevics, Martins
supporting information; experimental part, p. 2525 - 2528 (2011/11/13)
The first example of copper-catalyzed intramolecular N-arylation of hydroxamic acid derivatives is presented. Based on this transformation a new method for the synthesis of N-alkoxyindol-2-ones from 2-(2-bromoaryl) acetylhydroxamates has been developed. T